Antagonists of the Kv1.5 potassium channel

Amy L. Firth, Jason X.J. Yuan

Research output: Contribution to journalReview article

1 Scopus citations

Abstract

Potassium channels are an extensive family of ion channels selectively permeable to potassium ions (K+). They serve important functions in many crucial physiological processes and their dysregulation is key in several pathophysiological states, including pulmonary arterial hypertension, cancer and cardiac arrhythmias. One subset of K+ channels is comprised of the voltage-gated K+ (Kv) channels, of which over 40 isoforms have been identified and shown to serve important roles in cellular processes, such as the maintenance of resting membrane potential, cell contractility, neuronal activity and cell proliferation. The Kv1.5 isoform, encoded by the KCNA5 gene, has received much attention, with extensive research already carried out into its physiological, biophysical, structural and molecular properties. It is believed to be a potential target in diseases such as atrial fibrillation and pulmonary hypertension. As a result, a wide variety of pathways and pharmacological tools/drugs with modulatory effects on this channel have been identified. This review focuses on inhibitory regulation of Kv1.5 channels and will outline the following aspects: 1) structure, sequence and function; 2) transcriptional regulation; 3) trafficking; 4) occlusion/inhibition; and 5) altered kinetics or biophysical properties.

Original languageEnglish (US)
Pages (from-to)31-47
Number of pages17
JournalDrugs of the Future
Volume33
Issue number1
DOIs
StatePublished - Jan 1 2008
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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